Cholesterol lowering plants_Farkas

Lowering blood cholesterol
level with medicinal plants
Role of cholesterol
• cell membranes
• biosynthesis of steroids:
– animals: steroid hormones, bile acids, vitamin D,
ecdisteroids
– plants: steroid saponins, digitaloids, pregnane
derivatives, ecdisteroids
• transport, uptake: lipoprotein bound:
– HDL
– LDL
– VLDL
Lowering cholesterol level with herbs
• prevention
• already  cholesterol elvel – diet: 10% 
• , maintaining cholesterol level: nutrition plants
– cholesterol transfer within the body
– metabolism (absorption, circulation,
resynthesis)
• vs. statins: 20-35% , combinatory products
50-60% 
Csupor D., Szendrei K. (2009): Koleszterin és a gyógynövények. Gyógyszerészet
53: 142-151.
Lowering cholesterol level with herbs
• Plant sterins and sterin-containing plants:
sitosterin, soy, cereal sprouts, plant oils, oily seeds
• Plants slowing down the absorption of
cholesterol:
plant fibers, plants rich in fibers
• Plants inhibiting cholesterol synthesis:
garlic, artichoke, red rice
• Plants rich in unsaturated fatty acids, plant oils
and fish oils
• Natural antioxidants, plants rich in antioxidants
Csupor D., Szendrei K. (2009): Koleszterin és a gyógynövények. Gyógyszerészet
53: 142-151.
Allii sativi bulbus
Ph. Hg. VIII. / Ph. Eur.:
• Allii sativi bulbi pulvis
• Allium sativum ad
preparationes homeopathicas
Allii sativi bulbus effects, active compounds
• Effect: against atherosclerosis, high blood pressure,
antibacterial, antifungal
Garlic – cholesterol level 
• cholesterol: liver – de novo synthesis
– enzyme determining rate of synthesis:
HMG-CoA-reductase
(3-hydroxy-3-methyl-glutaryl-CoA-reductase)
– inhibition – several drugs (e.g. statins)
– garlic, artichoke, red rice
Garlic – human studies
• epidemiological data – total cholesterol level 
• several clinical studies:
garlic (or garlic powder, garlic extract) lowers cholesterol
level significantly more effectively compared to placebo
• metaanalyses:
– 6 randomised, placebo controlled study:
• total cholesterol concentration: 9,9% 
• LDL concentration:
11,4% 
• trigliceride concentration:
9,9% 
• HDL concentration:
11,5% 
• Alder, R., Lookinland, S., Berry, J.A., Williams, M.: J Am Acad Nurse Pract. 15. 120-129. (2003)
• Sobenin, I.A., Andrianova, I.V., Demidova, O.N., Gorchakova, T., Orekhov, A.N.: J Atheroscler Thromb. 15. 334338. (2008)
Human studies
Effect of garlic-containing herbal products on total cholesterol level (mmol/L)
￭ single studies, ￭ size: weight of study in metaanalysis
 in summary, – 95% CI
Forrás: Khoo Y.S.K., Aziz Z. (2009): J. Clin. Pharm. Ther. 34: 133-145.
Herbal products with garlic
• Circulin dragee
– preventing cardiovascular changes
accompanying ageing
• Esterin tablet (Medicaginis sativae folii
extr. sicc. (5:1), (standardised for 39.6-58.0
mg saponin content)
– significant decrease in blood
cholesterol level after 5-8 weeks
• Kwai garlic dragee
– Against atherosclerosis, enhances
circulation and heart functions
Allii ursini herba
Allium ursinum L. (Alliaceae / Liliaceae)
Allii ursini herba
• comparable effect to that of garlic – inhibition of cyclooxygenase enzyme and
platelet aggregation
• fewer clinical studies
• animal tests: similar therapeutic value
Cynara scolymus
artichoke
Cynara scolymus - artichoke
• as food – inflorescence bud
• medicine:
– leaves (Cynarae folium) – dried
– fresh buds → sap (juice)
• active compounds: caffeic acid derivatives:
– cynarin – most effective
– sesquiterpene-lactones (e.g. cynaropicrin)
Cynara scolymus - artichoke
• therapy: appetiser, cholagogue – lowers
blood cholesterol level
• cholagogue – caffeic acid derivatives,
!plant extract is more effective than cynarin
• HMG-CoA-reductase inhibition – flavonoids
(luteolin, cynaroside)
• choleretic – excreted bile acids are resupplemented from blood cholesterol
• strong antioxidant
Artichoke – human studies
• Majority: choleretic activity, few: cholesterol level 
• Metaanalysis: 2 randomised, controlled study:
artichoke  cholesterol level slightly, but significantly
Pittler, M.H., Thompson, C.O., Ernst, E.: Artichoke leaf extract for treating
hypercholesterolaemia. Cochrane Database Syst Rev. 2002
• patients with hypercholesterinaemia – treatment
with artichoke
→ total cholesterol level significantly 
→ changes in HDL-, LDL- and trigliceride concentration
are not significant
Bundy, R., Walker, A.F., Middleton, R.W., Wallis, C., Simpson, H.C.:
Phytomedicine 15, 668-675 (2008)
Artichoke in therapy
• in itself is not suitable for lowering already
existing high cholesterol levels
• ! prevention of atherosclerosis
• efficacy does not reach that of most
frequently applied drugs (statins)
• ! good quality herbal products, in appropriate
dose – can be similarly effective
• mild adverse effects
Gallexier herbal
bitter
indication: lowering of cholesterol level is not included
Red rice
Fermented with:
Monascus purpureus
Main active compound:
monacholin K = lovastatin
inhibitor of HMG-CoA
reductase enyzme – statins
Clinical studies:
• 4 randomised studies
• altogether 695 hyperlipidaemic or healthy individuals
• significant improvent – vs. placebo or compared to
starting cholesterol levels:
16-31% total cholesterol level 
21-32% LDL-level 
Thompson Coon, J.S., Ernst, E.: Journal Fam. Pract. 52, 468-478 (2003)
Trigonellae foenugraeci semen
AC: mucilageheteropolisaccharide
(galactomannane), protein, oil,
N-methyl-nicotinic acid,
trigonellin, steroid saponins
Appl: roborant, tonic, aromatic,
carminative, antiphlogistic,
Folk medicine: blood sugar ,
anti-atherosclerotic, enhances
production of breast milk
Trigonella foenum-graecum L.
(Fabaceae)
Ph.Hg. VIII.
Trigonellae foenugraeci semen
• Seed coat: bitter substance – excretion of bile acids
• Saponins + fiber content: inhibit the absorption of
bile acids and cholesterol
→ plasma cholesterol level 
• Special amino acid: 4-hydroxy-isoleucine
preclinical study:
– significantly  blood sugar and cholesterol level
• Current knowledge:
– suitable for normalising slightly increased levels of blood
sugar and cholesterol, as adjuvant in therapy
– no generally accepted therapeutic dose
Plantaginis ovatae semen,
Plantaginis ovatae seminis tegumentum
Plantago ovata Forssk.
(Plantaginaceae)
desert indianweed
AC: mucilage
heteropolysaccharide, oil,
protein, iridoid (aucubin)
Therapy: laxative (with plenty of
fluids), blood lipid level 
Ph. Hg. VIII.
Psyllii semen
Plantago afra L.(Plantago psyllum L.) - psyllium,
P. indica L. (P. arenaria W. et K.) – indianweed
(Plantaginaceae)
Plantago afra – psyllium
AC: mucilageheteropolysacchari
de, iridoid aucubin
Therapy: laxative,
cholesterol level 
Ph. Hg. VIII.
Plantago seeds – clinical studies
• several randomised clinical studies + metaanalysis:
–
–
–
–
total cholesterol level:
5-15% 
LDL concentration:
10-20% 
some studies: HDL plasma concentration 
compared to synthetic drug (lovastatin) : lower intensity
of effect
– ! 10 mg simvastatin + 15 g psyllium seed:  cholesterol
level at the same rate as 20 mg simvastatin
• Plantago seeds: adjuvant treatment
• Adverse effect: higher dose – diarrhoea
• Brown, L., Rosner, B., Willett, W.W., Sacks, F.M.: Am J Clin Nutr. 69, 30-42 (1999).
• Solà, R. et al. Am J Clin Nutr. 85, 1157-1163 (2007).
Herbal products:
cholesterol level lowering is not among
the accepted indications
Dietary supplements:
„health claims”:
maintains normal blood
lipid levels
Cyamopsidis seminis pulvis
(guar bean powder),
Guar galactomannanum
(guárbab galactomannan)
Cyamopsis tetragonolobus (L.) Taub.
(Fabaceae)
guar bean
Near-East, India, Africa
Seeds in the legume
AC: galactomannan guaran
Therapy: highly viscous  appetite,
in certain types of diabetes as
adjuvant,
 cholesterol levels,
cosmetic industry
Ph. Hg. VIII.
Guar bean
Human evidence:
slight hyperlipidaemia:
daily 10-25 g guar
bean powder:
•  blood lipid levels,
• improves the ratio of
LDL/HDL,
•  fat removed with
faeces
• Indication, dosage:
– powder (granulate,
tablet)
– serum lipid level (and
blood sugar level) 
– daily dose: 3 x 5 g bean
powder or product
corresponding to this
– increased fluid intake!
Adverse effects:
• mild hypoglycaemic symptoms
• may prolong the time needed for the absorption of other drugs
Medicago sativa – alfalfa
Fabaceae
• alfalfa saponins (pentacyclic triterpene
saponins) + cholesterol steroid-saponins
→ complex (intestines) → removed from
the body
•Esterin tablet
(Medicaginis sativae folii extr. sicc. (5:1),
(standardised for 39.6-58.0 mg saponin
content)
Oenothera biennis, O. erythrosepala
evening primrose oil:
advantageous fatty acid
composition (ω-6 fatty acids:
linolic acid, -linolenic acid)
cardiovascular disease
-6-desaturase enyzme:
•metabolism of essential fatty acids
• high cholesterol level, diabetes – reduced
activity
• ageing – activity 
Products containing evening
primrose oil
„Replacing saturated fatty acids with unsaturated fatty acids
has a beneficial effect on the total cholesterol level and LDL
level of blood.
„For prevention of cardiovascular diseases, for complementing therapy with
synthetic drugs, reduces high blood cholesterol levels, and the tendency for
thrombosis, slightly decreases blood pressure.”